Antileukaemic agent

Regioselective Acylation of Drug Intermediate for an Antileukaemic Agent... 

Some natural products contain an aziridine ring, e.g. mitomycins (3 mitomycin C). This is responsible for the cytostatic and antitumour activity of these antibiotics. Many synthetic aziridines have been screened for their antitumour activity. Some have reached the clinic, especially as antileukaemic agents, e.g. 4 and 5. 

NBD-Q was noted as a possible fluorescent label during the examination of benzofurazans as potential antileukaemic agents and blockers of thiol groups [192]. NBD-Q is prepared by nitrating 4-chlorobenzofurazan [193], It is commercially available. NBD-CI is a stable, non-fluorescent pale yellow solid, m.p. 97 °C, readily soluble in organic solvents and somewhat more soluble in water than Dns-CI. 

C10H12CIN5O3 285.689 Antileukaemic agent. Nucleoside transporter substrate. Cryst. (EtOH). Mp 220° softens. Log P -1.57 (calc). Resolidifies and browns on further heating. 

Isol. from the mushroom Xerocomus nigromaculatus of unknown palatability. Antineoplastic and antiviral agent, inhibits synth. of DNA, antileukaemic agent. Nucleoside transporter substrate. 

C11H13N3O5 267.241 Inhibits Pneumocystis carinii in vitro and in vivo. Purine nucleoside phosphorylase inhibitor. Antileishmanial and potential antileukaemic agent. Struct, originally assigned to Pyrrolosine, P-117. 

C32H53NO22 803.764 Heteroglycan antibiotic. Polymeric. Minimum formula given. Isol. from Alcaligenes latus. Antileukaemic agent. [a]o -13 (c, 1 in O.IM NaOH). Hayakawa, Y. et al, Agric. Biol Chem., 1985, 49, 2437 2443 (isol struct, props)... 

Nucleoside antibiotic. Isol. from the mushroom Clitocybe nebularis (clouded agaric), from Streptomyces yokosukaen-sis and Microbispora sp. nov. Shows tuberculostatic and antimitotic activity. Adenosine deaminase inhibitor. Investigated as an antileukaemic agent in combination therapies. Needles (MeOH). 

C13H16N6O4 320.307 Antineoplastic, antileukaemic agent. Possesses anti-HIV activity. In Phase II clinical trials (1993). Found to be ineffective and had unacceptable toxic effects... 

An improved synthesis of the antileukaemic agent l-/S-D-arabinofuranosyI-cytosine (397) is shown in Scheme 80. Ethyl 3,5,6-tri-0-acetyl-2-5 -ethyl-... 

Clinically important drugs, such as methotrexate 4-amino-lO-methyl folic acid MTX - which has considerable significance as an antileukaemic agent can be assayed using chemiluminescence immunoassay methods, coupling the drug with firefly luciferase. 

Some positional isomers of coralyne have been synthesized and examined for antileukaemic activity,82 and the distribution of salts of coralyne after they have been administered to rodents has been studied.83 Dehydrogenation of canadine to berberrubine (59) can be accomplished in ethylene glycol and hydrochloric acid with palladium or with tris(triphenylphosphinyl)rhodium chloride, the reaction proceeding faster at low temperatures with the latter catalyst.84 Derivatives of 13-methylberberrubine and its analogues have been synthesized, so that they might be screened to find their potential as antitumour agents.85... 

Wani, M.C., Taylor, H.L., Wall, M.E. Plant Antitumor agents colubrinol acetate and colubrinol, antileukaemic ansa macrolides from Colubrina texensis. J. Chem. Soc. Chem. Comm. 1973, 390... 

Isol. from Tolypothrix conglutinata var. colorata. Shows antileukaemic props. Antifungal agent and cy to toxin. Amorph. solid. 

Wani MC, Taylor HL, Thompson JB, Wall ME, McPhail AT, Onan KD (1979) Plant antitumour agents-XV Isolation and x-ray crystal structure of a new antileukaemic quassinoid undulatone from Hannoa undulate. Tetrahedron 35 17-24... 

Wani, M. C., H. L. Taylor, J. B. Thompson, M. E. Wall, A. T. McPhail, and K. D. Onan Plant Antitumour Agents. XV. Isolation and X-Ray Crystal Structure of a New Antileukaemic Quassinoid Undulatone from Hannoa Undulata. Tetrahedron 35, 17... 

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